27results about How to "Small side effects" patented technology

The application relates to a benzene ring-containing compound with analgesic efficacy, a preparation method and use thereof, and relates to the field of medicinal chemistry. The compound is a compound shown in formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a crystal form thereof, or a prodrug thereof, or a metabolite thereof, or a deuterium derivative thereof. The analgesic effect of the compound is excellent, the compound is safe to use, has small toxic and side effects, and does not produce dependence during use. Therefore, the compound has a wide application prospect in the preparation of analgesic drugs, and provides a new selection for preparing drugs with analgesic action in the clinic.

This invention provides a mulberry leaf and wolfberry composition, comprising aqueous extracts of wolfberry, mulberry leaves, astragalus, yam, kudzu root, and green tea. This invention also provides oral preparations and food products containing this composition. Furthermore, this invention provides the application of the composition or oral preparation in the preparation of health foods that help maintain healthy blood sugar levels and hypoglycemic drugs. The composition provided by this invention has the effect of lowering blood sugar, and the selected raw materials are highly safe, have few toxic side effects, and are widely available, possessing significant market value and development prospects.

The application relates to the biological field, in particular to a lactobacillus fermentum zhangweizhuang cell lysate for regulating macrophage polarization and assisting PD-1 inhibitor to inhibit liver cancer development. The ZW18 cell lysate is a cell lysate containing various metabolites prepared from lactobacillus fermentum ZW18 with a preservation number of CGMCC No. 23549 through fermentation, heat treatment and ultrasonic lysis treatment, and the metabolites at least contain active ingredients: extracellular polysaccharide of greater than or equal to 2200 mg / L, amino acid of greater than or equal to 70 mmol / L and flavonoid of greater than or equal to 150 g / L. The ZW18 cell lysate can induce M1 type polarization of macrophages, can assist PD-1 inhibitor to inhibit liver cancer development in cooperation with the PD-1 inhibitor, can regulate intestinal flora imbalance caused by liver cancer, and can be used for preparing a combined preparation with the PD-1 inhibitor.

This invention relates to the field of organic polymer adhesives, specifically disclosing a modified castor oil polyurethane adhesive containing catalytic groups, its preparation method, and its application. The adhesive is a two-component compound. By weight, component A comprises 30.0-50.0 parts modified castor oil and 0.0-30.0 parts refined castor oil; component B comprises 30.0-50.0 parts polyisocyanate or a modified polyisocyanate and 0.00-0.05 parts dehydrating agent. The modified castor oil is prepared by first reacting refined castor oil and cysteine ​​hydrochloride via a mercapto-olefin addition reaction, followed by neutralization with a strong base. The modified castor oil simultaneously contains hydroxyl, amino reactive groups, and quaternary ammonium salt catalytic groups, exhibiting rapid reaction with isocyanate groups. The mixture of the two components exhibits certain thixotropy, and the crosslinked product has high strength.

This invention provides a traditional Chinese medicine composition for treating viral pneumonia in calves, its preparation method, and its application, belonging to the field of veterinary drug technology. The traditional Chinese medicine composition provided by this invention comprises the following raw materials in parts by weight: 15-20 parts of Gentiana scabra, 15-20 parts of Gardenia jasminoides, 15-20 parts of Scutellaria baicalensis, 10-15 parts of Bupleurum chinense, 25-35 parts of Rehmannia glutinosa, 25-35 parts of Plantago asiatica, 15-20 parts of Alisma plantago-aquatica, 25-35 parts of Akebia trifoliata, 10-15 parts of Angelica sinensis, 25-35 parts of Smilax glabra, 15-20 parts of Dioscorea hypoglauca, 25-35 parts of Dictamnus dasycarpus, and 10-15 parts of Glycyrrhiza uralensis (processed). The traditional Chinese medicine composition of this invention can effectively treat viral pneumonia in calves, and also has advantages that antibiotics cannot possess, such as being green and safe, residue-free, having few toxic side effects, low cost, convenient production, and being less likely to produce drug-resistant bacteria.

The application provides application of tanshinone or a derivative thereof in preparation of a monkeypox virus resisting drug. In a cell model infected by the monkeypox virus, production of infectious virus particles can be significantly reduced. In a mouse infection model, Tanshinone VII can effectively reduce pathological damage of lung tissues and improve survival rate of animals. The above evidence indicates that Tanshinone VII has potential efficacy in resisting the monkeypox virus. It is inferred that tanshinone or the derivative thereof can play a double role in resisting the monkeypox virus and host protection.

The invention belongs to the technical field of traditional Chinese medicines, and particularly provides a traditional Chinese medicine composition for treating hepatic fibrosis and a preparation method thereof. According to the invention, astragalus membranaceus, vinegar-processed curcuma zedoary, salvia miltiorrhiza, moutan bark, radix paeoniae rubra, angelica sinensis, curcuma aromatica, fructus amomi, bran-fried atractylodes macrocephala koidz, poria cocos, fingered citron, vinegar-processed bupleurum chinense and honey-fried licorice root are adopted as raw materials and are subjected to proper weight proportioning; wherein the astragalus membranaceus is a monarch drug, and the vinegar curcuma zedoary, the salvia miltiorrhiza, the moutan bark, the red paeony root, the angelica sinensis, the radix curcumae, the fructus amomi and the bran-fried rhizoma atractylodis macrocephalae are The vinegar bupleurum chinense, fingered citron and poria cocos are used as adjuvant drugs, and the liquorice is used as conductant drug; all the medicines are combined to achieve the effects of replenishing qi to invigorate the spleen, soothing the liver, regulating qi and promoting blood circulation to remove blood stasis. Under the synergistic effect of all the medicine components, the traditional Chinese medicine composition has a good curative effect on liver fibrosis, especially liver fibrosis common clinically with liver depression, spleen deficiency and blood stasis syndromes, and is small in toxic and side effect and worthy of clinical application and popularization.

The application provides a pyrido[4,3-d]pyrimidine compound with a structure shown in formula I or a pharmaceutically acceptable salt or a stereoisomer thereof, and an application thereof. The pyrido[4,3-d]pyrimidine compound provided by the application is a molecular glue degrader for KRAS mutants, can effectively degrade mutant KRAS, thereby effectively inhibiting the activity of KRAS mutants, can effectively inhibit the proliferation of tumor cells caused by KRAS mutation, has good selectivity, small toxic and side effects, good safety, provides a potential KRAS mutant degrading therapeutic drug for KRAS mutant cancer patients, explores a novel high-efficiency E3 ubiquitin ligase for KRAS mutant proteins, and is expected to develop a novel E3 ubiquitin ligase ligand. Formula I

The invention belongs to the technical field of traditional Chinese medicines, and particularly relates to a traditional Chinese medicine composition capable of eliminating pulmonary nodules and a preparation method thereof. The traditional Chinese medicine comprises astragalus membranaceus, codonopsis pilosula, poria cocos, roasted rhizoma atractylodis macrocephalae, honey-fried licorice root and the like, treats both symptoms and root causes, breaks through the limitation of traditional pulmonary nodule treatment, and can accelerate blood flow and condition physique while treating pulmonary nodule; the traditional operation method is broken through by eliminating phlegm, removing dampness, promoting blood circulation to remove blood stasis and softening hardness to dissipate stagnation, and pulmonary nodules caused by imbalance of viscera and imbalance of yin and yang can be adjusted; according to the traditional Chinese medicine composition, a plurality of medicines are combined and comprehensively attacked, the lung function is improved, yin-yang balance is corrected, and nodules are eliminated.

This invention discloses a thiadiazolidinone compound with PTPN2 / PTPN1 inhibitory activity, its preparation method, and its applications, belonging to the field of medicinal chemistry. The thiadiazolidinone derivative described in this invention is a compound with the structure shown in general formula (I) or a pharmaceutically acceptable salt thereof. This invention also discloses the application of the above-mentioned thiadiazolidinone derivative in drugs for treating PTPN2 / PTPN1-mediated diseases. The compound disclosed in this invention has significant inhibitory activity against PTPN2 / PTPN1 phosphatases, and has an important influence on tumor development and immune response. It can also be used in combination with immunosuppressants to treat related immune diseases. It can be developed into an antitumor drug with high activity, good selectivity, and low toxicity, and has the characteristics of high plasticity and great potential for future modification.

The application belongs to the field of biological medicine, and discloses a pharmaceutical composition of water channel protein inhibitor combined with temozolomide for treating brain glioma, wherein the pharmaceutical composition comprises AQP4 inhibitor AER270 and TMZ. The application further discloses a pharmaceutical preparation comprising the above pharmaceutical composition and application of the pharmaceutical preparation in preparation of a medicine for treating brain glioma. The composition provided by the application provides an effective drug combination strategy for treating brain glioma, and it is found for the first time that AER270 and TMZ have a synergistic effect on the treatment of brain glioma.

The application discloses a use of hyperoside in resisting equid herpesvirus 8 (EHV-8) infection. Through qPCR, Western Blot and other experimental techniques, it is revealed on multiple levels that the hyperoside can significantly inhibit the replication of EHV-8, and the mechanism of the hyperoside in resisting the EHV-8 infection is clarified from the aspect of blocking the internalization of the EHV-8, so that the hyperoside can be applied in preparing an anti-EHV-8 medicine.

The application discloses a 5,6-diphenylpyrazine-2-azacycle compound and a preparation method and application thereof. The 5,6-diphenylpyrazine-2-azacycle compound is synthesized by a more simple and economical method, and it is found through anti-platelet aggregation activity detection that the prepared 5,6-diphenylpyrazine-2-azacycle compound has excellent anti-platelet aggregation activity and small toxic side effect, and can be used as an active ingredient of an antithrombotic drug. In addition, the activity of the synthesized 5,6-diphenylpyrazine-2-azacycle compound is greatly influenced by chiral compounds, and the activity of an R-type compound is obviously greater than that of an S-type compound, so that the R-type compound can play a more excellent antithrombotic effect as an active ingredient of an IP receptor agonist or other antithrombotic drug.

The invention belongs to the field of biological medicine, and discloses a pharmaceutical composition combining an aquaporin inhibitor and temozolomide for treating brain glioma, and the pharmaceutical composition comprises an AQP4 inhibitor AER270 and TMZ. The invention further discloses a pharmaceutical preparation containing the pharmaceutical composition and application of the pharmaceutical preparation to preparation of drugs for treating brain glioma. The composition provided by the invention provides an effective drug combination strategy for treatment of brain glioma, and it is found for the first time that the combination of AER270 and TMZ has a synergistic effect on treatment of brain glioma.

The invention relates to a carbonic anhydrase IX protein targeted radiopharmaceutical, in particular to a compound shown as a formula (I), which can effectively target carbonic anhydrase IX protein, and has the advantages of high in-vivo metabolism speed, high specificity, small intake in non-target organs, small toxic and side effects on the non-target organs, convenience in imaging and high safety. And the compounds can be used for diagnosing or treating diseases for overexpressing the carbonic anhydrase IX protein. (I)

The application belongs to the technical field of medicine, and particularly relates to application of phyllangin in preparation of anti-senecavirus virus (SVV) drugs. The phyllangin is separated from seeds of phyllanthus emblica, and the purity of the phyllangin reaches more than 99%. The effective concentration of the phyllangin in the anti-SVV drug is in the range of 1-20 muM. The application further provides a preparation for treating SVV, and the preparation comprises an active ingredient of phyllangin. The application firstly finds that the phyllangin has the effect of resisting SVV, the phyllangin as a natural product has low cytotoxicity to host cells, has small toxic and side effects, and has a relatively wide source, and the application of the phyllangin to preparation of anti-SVV drugs provides a new choice for treatment of SVV infection.

This application relates to the field of biomedical technology, and in particular to the application of N-acetylneuraminic acid in the preparation of drugs for treating methamphetamine addiction. This application is the first to discover the key role of N-acetylneuraminic acid (Neu5Ac) in the treatment of methamphetamine addiction, which can significantly reduce the CPP score in methamphetamine-addicted mice, demonstrating a good therapeutic effect on methamphetamine addiction. Furthermore, Neu5Ac can be synthesized endogenously, exhibiting advantages such as good biocompatibility and low toxicity.

This invention relates to the field of veterinary preventive and therapeutic drugs. The invention provides a traditional Chinese medicine composition for the prevention and / or treatment of porcine reproductive and respiratory syndrome (PRRS) and its preparation method, comprising the following components: Indigo naturalis, Forsythia suspensa, Arctium lappa, Dryopteris crassirhizoma, Lithospermum erythrorhizon, Taraxacum mongolicum, Rheum palmatum, Scutellaria barbata, Glycyrrhiza uralensis, Hordeum vulgare, Bupleurum chinense, and Terminalia chebula. The invention also provides a traditional Chinese medicine preparation comprising the aforementioned composition. Using the above-mentioned components in combination with the technical solution of this invention can effectively enhance the inhibitory effect on pathogenic microorganisms and the anti-PRRSV virus effect, improve immunity, and enhance the disease resistance of pigs; alleviate symptoms such as depression and loss of appetite caused by PRRSV, and regulate the gastrointestinal health of animals; at the same time, it has few toxic side effects and is less likely to induce drug resistance.

The present application relates to a kind of I type photosensitizer based on squarylium and its preparation method and application, belong to the preparation of chemical material and biomedical nanomaterial technical field.The I type photosensitizer provided by the present application, its molecular structure is with tetraphenyl ethylene substituted indoline derivative as donor, with square acid as acceptor.The rotor structure of tetraphenyl ethylene can effectively avoid the close π-π stacking between molecules.The I type photosensitizer of the present application has the advantages of high molar absorption coefficient, good light stability and low biological toxicity, and also shows the efficient I type active oxygen (·OH) generation capacity and photo-thermal conversion capacity (54.2%), therefore it can be used for photodynamic / photothermal combined antitumor and antibacterial treatment.In photodynamic / photothermal combined treatment, after using laser irradiation, the I type photosensitizer can simultaneously generate a large amount of active oxygen (·OH) and heat, which can efficiently kill tumor cells and bacteria.

This invention relates to an abalone active peptide with the amino acid sequence DYPRPW. The preparation method is as follows: Abalone viscera are enzymatically hydrolyzed using alkaline protease to obtain an enzymatic hydrolysate; the enzyme is then inactivated after hydrolysis. The hydrolysate is centrifuged, coarsely filtered, and ultrafiltered to collect multiple polypeptides with a molecular weight less than 1 kDa, which are then freeze-dried into powder. The freeze-dried polypeptide powders are sequenced to obtain multiple polypeptide sequences; repetitive sequences are deleted, and multiple non-repetitive polypeptides are screened. Using the protein HMGR as a receptor, the obtained polypeptides are virtually screened using docking software, and the polypeptides with the highest docking scores are selected for solid-phase synthesis to obtain the abalone active peptide. This invention's abalone active peptide can effectively inhibit the accumulation of total cholesterol and total triglycerides in cells, exhibits a high inhibition rate of cholesterol micelle solubility, and has lipid-lowering effects. It can be used to prepare adjuvant lipid-lowering drugs, and compared with traditional lipid-lowering drugs, it has the advantages of high specificity and fewer toxic side effects.

The invention provides an aminothiocarbonyl compound, a preparation method thereof and application of the aminothiocarbonyl compound in preparation of drugs for preventing or treating toxoplasma gondii infection. In long-term research, the inventor finds that the aminothiocarbonyl compound shown in the formula has a remarkable inhibitory activity effect on intracellular parasitic protozoa toxoplasma gondii, has small toxic and side effects, and has the potential of preparing drugs for preventing or treating toxoplasma gondii infection. Meanwhile, the toxoplasma gondii resisting activity and cell safety of the compound TU-BO and the compound TU-BP are verified, and results show that the half effective inhibition concentrations of the TU-BO and the TU-BP on toxoplasma gondii are 1.478 mu M and 7.219 mu M respectively, the half cytotoxic concentrations of the TU-BO and the TU-BP on Vero cells are 61.73 mu M and 654.5 mu M respectively, and the safety indexes SI are 41.77 and 90.66 respectively. Compared with existing drugs for treating toxoplasma gondii infection, the effective inhibition concentration of TU-BO and TU-BP is far smaller than that of cytotoxicity, and the TU-BO and TU-BP can significantly inhibit lysis cells of toxoplasma gondii, inhibit invasion and proliferation of toxoplasma gondii, and have significant effects of preventing and treating toxoplasma gondii infection.

The present application relates to the technical field of biological medicine, and discloses a beta-galactoside enzyme activated AIE type photosensitizer and a preparation method and application thereof. The present application provides an AIE photosensitizer, which is a compound (1) with a structural formula as shown in formula (1). When the galactose group exists, the power supply group is shielded, the ICT effect is weakened, and the PDT performance is in a closed state. When the galactose group is hydrolyzed by beta-galactosidase, the overall water solubility of the compound (1) from which the galactose group is hydrolyzed becomes poor, and the compound (1) is aggregated. Meanwhile, the power supply group hydroxyl is opened, the ICT effect is enhanced, and the PDT performance is in an open state. The glycosidase activity in ovarian cancer cells is abnormally increased, and the glycosidase in ovarian cancer cells triggers the AIE photosensitizer to be activated in the tumor microenvironment with high glycosidase activity, so that precise positioning is achieved. This selective activation mode significantly reduces the misactivation of the photosensitizer in normal tissues and reduces the damage to healthy tissues.

The application discloses a kind of pyranose derivatives represented by the following general formula I, its stereoisomer, pharmaceutically acceptable salt, crystalline hydrate or solvate, its preparation method, the pharmaceutical composition for protecting the compounds and its application in central nervous system diseases and inflammatory diseases etc..According to the pyranose derivative of the application, the cell viability of A beta 1-42 induced cell damage model is significantly improved, the cell viability of 6-hydroxydopamine induced cell damage model is improved, the cell viability of oxygen-glucose deprivation / reoxygenation cell damage model is improved, the level of lipopolysaccharide induced cell inflammatory factor is inhibited, etc.The pharmacological effects have good clinical application prospect.

This invention provides a reactive oxygen species (ROS)-activated nitrogen mustard prodrug, its preparation method, and its application. This invention belongs to the field of medicinal chemistry. By introducing ROS-sensitive groups into nitrogen mustard compounds, it maintains an inactive state in normal tissues, only becoming activated in the tumor microenvironment due to elevated ROS levels, releasing cytotoxic nitrogen mustard components. This ROS-activated nitrogen mustard prodrug not only overcomes the shortcomings of traditional nitrogen mustard drugs but also provides new directions and ideas for the development of antitumor drugs. Furthermore, this nitrogen mustard prodrug enriches the structural types of nitrogen mustard prodrugs, improves drug selectivity in tumor cells, and reduces toxic side effects.

The application discloses peanut meal treated by liquid nitrogen, and can obtain peanut alpha helix-loop peptides with broad-spectrum antifungal activity through separation. The peanut alpha helix-loop peptides with antifungal activity can effectively inhibit various plant pathogenic fungi (rust fungi, fusarium, colletotrichum and sordaria). The peanut alpha helix-loop peptides can effectively improve the antifungal activity of plants.

The application discloses application of clofazimine in preparation of a medicine for preventing and / or treating porcine epidemic diarrhea virus (PEDV) infection. The clofazimine is safe and has small toxic and side effects against the PEDV, provides a new direction for research and development of the medicine for preventing and / or treating the PEDV infection, and has important research significance and application significance for research and development of the medicine for preventing and / or treating the PEDV infection. The clofazimine presents a dose-dependent mode to inhibit replication of the PEDV, and provides a scientific and reliable theoretical basis for clinical treatment.

The application discloses an oral liquid for treating purpura, which is prepared by high-temperature extraction of red tea with yellow rice wine and clarification of the extracted liquid. The oral liquid is prepared by taking red tea and yellow rice wine as raw materials, can effectively treat thrombocytopenic purpura, allergic purpura and capillary bleeding caused by thrombocytopenia due to primary diseases, has small toxic and side effects and high efficiency, and is in the form of stable oral liquid, so that the oral liquid is convenient to take, carry and store.